Topical drying composition comprising encapsulated trehalose and method of using same

ABSTRACT

A topical drying composition is provided for removal of sweat from skin areas which are vulnerable to sweating after sweat producing activities. The drying efficacy of the composition is due to the presence of encapsulated trehalose, with or without aluminum used as aluminum zirconium compound. Application of an effective amount of the composition to the skin prior to exercise or sweat removal activity reduces sweating and accelerates drying of the skin.

FIELD OF THE INVENTION

The present invention relates generally to topical drying compositionsand is particularly related to topical drying compositions containing aneffective amount of encapsulated trehalose. In one aspect, thisinvention relates to a topical drying composition containing aneffective amount of encapsulated trehalose for enhancing drying of theskin when it is applied to the skin of persons, such as athletes, afterperspiration due to exercise such as playing tennis, golf, jogging,running, basketball or other sweat-producing aerobic activities. Inanother aspect, the present invention relates to topical compositioncontaining encapsulated trehalose and known aluminum compounds oraluminum-zirconium compounds.

The invention also relates to a method of using such topical dryingcompositions.

BACKGROUND OF THE INVENTION

Trehalose is a known non-reducing disaccharide composed of D₊glucoseunits. It is a white, odorless, sweet-tasting powder and, like maltose,is about 45% as sweet as sugar and has a very low hydroscopicity(moisture attraction). Trehalose is found in honey, bread, beer andseafood and there are several prior art patents relating to various usesof trehalose. For example, U.S. Pat. No. 4,839,164 discloses cosmeticcompositions containing trehalose which increase the penetration ofcertain therapeutically beneficial ingredients into the skin therebyenhancing the therapeutic effects of those ingredients on the skin. Thetrehalose is used in a pharmaceutically acceptable carrier and severaltrehalose-containing formulations are disclosed in said patent, such asshampoo formulations, hair-conditioning formulations, skin care gelformulations, lotions, and skin care creams.

U.S. Pat. No. 5,543,513 discloses the use of anhydrous trehalose as adesiccant for dehydrating various products such as dehydrated food aswell as dehydrated pharmaceuticals. High-quality food products havingreduced moisture content can be prepared by incorporating anhydroustrehalose into food products having relatively high moisture contentthereby converting the anhydrous trehalose into hydrous crystallinetrehalose.

U.S. Pat. No. 6,555,526 discloses an ophthalmic pharmaceuticalcomposition comprising trehalose as the effective ingredient. Asdisclosed in said patent, there are three types of optical isomers oftrehalose, i.e., ∝, ∝-trehalose, ∝, β-trehalose and β, β-trehalose. Allisomers exert therapeutic and/or prophylactic effect on signs of Sjorgensyndrome.

U.S. Pat. No. 6,723,170 discloses a crystalline trehalose dihydrate withlow hydroscopicity. Variety of uses are disclosed for the crystallinetrehalose dihydrate, including its use as a sweetener, taste-improvingagent, in feeds and pet foods for animals, in soaps, skin creams, bodyshampoos, hair creams, moisture-controlling agent and a host of otheruses disclosed in said patent.

Notwithstanding a variety of uses of trehalose disclosed in the priorart patents, none of them recognize the efficacy of trehalose for use intopical drying composition. In a commonly assigned, copendingapplication Ser. No. 12/214,863 filed Jun. 24, 2008, there is describeda topical drying composition containing an effective amount oftrehalose, in hydrous or anhydrous form. The composition describedtherein, whether in aqueous solution form or a cream, when applied tothe area of the skin which is vulnerable to perspiration, was effectivein drying the perspiration resulting from aerobic or other vigoroussweat-producing exercises. The aforementioned copending applicationdiscloses several trehalose-containing formulations which are effectivetopical drying compositions. Neither of the prior art patents, nor theaforementioned patent application disclose the use of encapsulatedtrehalose in formulations used for topical drying compositions and sweatremoval.

Therefore, it is an object of the present invention to use encapsulatedtrehalose in topical drying compositions.

It is a further object of the present invention to provide a moreeffective drying composition which includes encapsulated trehalose asthe effective ingredient for sweat removal.

It is another object of the present invention to provide a topicaldrying composition which contains encapsulated trehalose and knownaluminum compounds used in lesser quantities than have heretofore beenused in the prior art sweat removing drying compositions using onlyknown aluminum compounds.

It is also an object of the present invention to provide a method ofusing these compositions for topical drying and sweat removal.

The foregoing and other objects and advantages of the present inventionwill be appreciated from the ensuing detailed description and theillustrative examples.

SUMMARY OF THE INVENTION

A topical drying composition is provided for removal of sweat from theskin in areas which are vulnerable to sweating after sweat producingexercises such as playing tennis, golf, running, basketball, etc. Thecomposition of this invention comprises, as its effective component,encapsulated trehalose wherein trehalose particles are encapsulated in asuitable medium such as a solution of dimethicone 200. A suitableeffective composition comprises the following ingredients: trehalose,dimethicone, distilled water, Carbopol Ultrex 10, tetra sodium ethylenediamine tetra acetic acid, sorbitan monolaurate, cocoa butter,polysorbate 20 (Tween 20), Germal II (antibacterial agent), hyamine,bovine collagen (2% aqueous), elastin 2% aqueous (natural) and 10%sodium hydroxide to a pH of 6.4.

Another suitable composition which is effective for sweat removalincludes aluminum zirconium compound which contains far less aluminumthan has heretofore been used in prior art compositions. The drasticreduction in the amount of aluminum is due to the use of encapsulatedtrehalose in the composition.

The application of an effective amount of composition containingencapsulated trehalose, with or without an aluminum compound, results insweat removal from the skin. Volunteers applying an effective amount ofthe composition of this invention have experienced far less sweatingafter strenuous, normally sweat producing exercises.

DETAILED DESCRIPTION OF THE INVENTION

In accordance with this invention more effective sweat removal can berealized by using a composition which contains encapsulated trehalose ashereinafter described. The application of the composition of thisinvention to the sweating area of the skin effects removal of the sweator perspiration in a controlled and longer acting manner due tocontrolled rate of release of trehalose.

In the following description, the invention will be described and itseffectiveness will be shown by several examples which are intended to beillustrative but without limiting the invention. In order to prepare acomposition which is useful for the purpose of this invention, theencapsulated trehalose is first prepared separately as described below,wherein all parts are by weight.

An aqueous alginate solution of 1% by weight concentration is preparedby dissolving 0.25 sodium alginate in 25 grams distilled water.Thereafter, 25 grams of trehalose (obtained from Sigma Aldrich, St.Louis, Mo.) was added to the sodium alginate solution and dissolved at45° C. to form a 50% concentrated trehalose in the alginate solutions(solution A). Thereafter an aqueous calcium chloride solution wasprepared by dissolving 0.5 gm of calcium chloride in 50 gms distilledwater to form 1% weight solution (solution B). 25 grams of this calciumchloride solution was subjected to high shear mixing, at 1000 rpm, usinga rotator type homogenizer (Fisher Powergen 125, Fisher Scientific,Pittsburgh, Pa.). 50 grams of solution A was added to solution B underthe same high shear agitation to form a finely divided dispersed slurryof gelled particles of trehalose/calcium alginate in a continuousaqueous phase. 75 grams of this aqueous slurry is slowly added to 50grams of silicone fluid, DC200, having a viscosity of 100 centistokes(Dow Corning, Midland, Mich.) under the same high shear agitation toform water-in-oil dispersion. The formation of the dispersion wasfacilitated by adding 3 grams of sorbitan monooleate (Cognis,Cincinnati, Ohio) into the silicone fluid prior to addition of theaqueous compound. The resulting dispersion was further dispersed inwater and encapsulated as follows.

An aqueous solution of sodium carboxymethylcellulose CMC, Akucell AF1703 (Akzo Nobel, Netherlands) was prepared by dissolving 0.2 gm of CMCin 106.8 grams of distilled water. To this CMC solution was added 2.5grams of Tween 20, polyoxyethylene 20 sorbitan monolaurate (Croda,Edison, N.J.) and 2.5 grams of sorbitan monooleate and the solution wasstirred in a magnetic stirrer at 500 rpm. Thereafter, the entire 128 gmsof the trehalose/alginate/silicone dispersion is added to the CMCsolution to form a dispersion of silicone phase wherein droplets ofsilicone oil contain dispersed particles of trehalose/alginate.

The resulting trehalose encapsulated composition is as follows:

Component Weight (g) Weight % Sodium Alginate 1% soln 25.0 10.00%Trehalose 25.0 10.00% Calcium Chloride 1% soln 25.0 10.00% Dimethicone200 50.0 20.00% Span 80 5.5 2.20% Sodium carboxymethylcellulose 0.20.08% Tween 20 2.5 1.00% Cetrimonium chloride 1% soln 10.0 4.00% Water106.8 42.72% Total 250 100.00

Independently from preparation of the encapsulated trehalose, thefollowing mixture was prepared and mixed with encapsulated trehalose.

450 grams of distilled water was charged to a reaction vessel equippedwith a stirrer, at room temperature and combined pressure and 3.4 gramof Ultrex 10, a polyacrylic acid thickener, available from B.F. GoodrichCo., was added to the reaction vessel and mixed thoroughly with thewater. Thereafter, 2 grams of tetra sodium ethylene diamine tetra aceticacid was added to the reaction vessel with continuous agitation. Theresult was a gel which was heated to 50° c.

Another mixture was also prepared containing 38 gm sorbitan monolaureateand 11.4 grams of polysorbate 20 and 31 grams cocoa butter, and themixture heated to 50° c. with continuous agitation.

The above two mixtures were then combined slowly forming a creamyhomogenous mixture and cooled to room temperature. The creamy mixturehad the following composition:

Ingredients Weight gm Weight % Distilled water 450 84 Carbapol Ultrex 10⁽¹⁾ 3.4 0.63 Tetra Sodium (DETA) 2.0 .37 Cocoa butter 31 5.78 Sorbitanmonolaurate 38 7.09 Polysorbate 20 (Tween 20) 11.4 2.13 TOTAL WEIGHT535.8 100.00 ⁽¹⁾ carboxy polymethylene

The encapsulated composition which was formed as previously describedwas the then mixed with the above creamy composition. The finalencapsulated formula has the following composition.

Ingredients Weight % Trehalose 3.30 Dimethicone 6.60 Distilled water79.36 Carbopol Ultrex 10 .20 Tetra sodium ethylene diamine tetra aceticacid .13 Sorbitan monolaurate 2.50 Cocoa butter 2.00 Polysorbate 20(Tween 20) .76 Germal II (antibacterial agent) .15 Hyamine 2.10 Bovinecollagen 2% aqueous 2.00 Elastin 2% acqueous (natural) 1.00 10% sodiumhydroxide to a pH of 6.4 TOTAL 100Clinical Test

The encapsulated formula hereinbefore described was tested for its sweatremoval efficacy. Three males and three female volunteers were tested.The ages and weight of the males and females are listed below.

All subjects cleaned their armpits thoroughly and then applied thecomposition as a cream to both armpits using their finger tips. Eachvolunteer was given six-one gram sample and instructed to apply thecream to the armpit and report the degree of sweating and odor afterexercise.

Males Females 1. Age 25, weight 165 lbs. 1. Age 24, weight 110 lbs. 2.Age 42, weight 185 lbs. 2. Age 35, weight 125 lbs. 3. Age 51, weight 250lbs. 3. Age 50, weight 150 lbs.Results in Males

1. No sweating or odor was reported by volunteer #1 after 2 hours ofweight lifting followed by 15 minutes in a sauna

2. Insignificant sweating was observed after running for 5 miles in 70°F. weather.

3. Minimal sweating and odor were reported by volunteer #3 after threehours outdoors in hot, humid weather (85° F.).

Results in Females

1. Minimal sweating but some odor was reported after running 3 miles ona treadmill.

2. Some sweating was reported with no odor after performing strenuousaerobic exercise for 45 minutes. Minimal sweating and odor on secondday.

3. No sweating was observed after working from 9:00 A.M. to 5:00 PM, andno tackiness reported.

In another embodiment of this invention aluminum may be added to theencapsulated formulation hereinbefore described. The aluminum is addedas aluminum compound or aluminum-zirconium compound such as, forexample, aluminum chlorohydrate, aluminum chlorohydrex polyethyleneglycol, aluminum chlorohydrex propylene glycol, aluminumdichlorohydrate, aluminum dichlorohydrex polyethylene glycol, aluminumdichlorohydrex propylene glycol, aluminum sesquichlorohydrate, aluminumsesquichlorohydrex polyethylene glycol, aluminum sesquichlorohydrexpropylene glycol, aluminum zirconium octachlorohydrate, aluminumzirconium otachlorohydrex gly, aluminum zirconium pentachiorohydrate,aluminum zirconium pentachlorohydrex gly, aluminum zirconiumtetrachlorohydrate, aluminum zirconium tetrachlorohydrex gly, aluminumzirconium trichlorohydrate, aluminum zirconium trichlorohydrex gly,buffered aluminum sulfate, potassium aluminum, sodium aluminum,chlorohydroxy lactate aluminum sesquichlorohydrates, sodium aluminumlactate, or mixtures thereof.

The use of small amounts of aluminum in the composition of thisinvention reduces the required quantity of trehalose without adverselyaffecting the sweat removal efficacy of the composition. The followingexamples describe the preparation of such aluminum-containingcompositions, these examples are intended to be illustrative withoutlimiting the invention. The aluminum compound used in these examples waspharmaceutical grade aluminum zirconium tetrachlorohydrox gly.

Example 1

2.8 grams of the aluminum compound and 0.7 gm of hyamine were dissolvedin distilled water and the solution was then combined with 121 gms ofthe encapsulated composition previously described, forming a homogenouscream. 20 percent sodium hydroxide solution was then added to themixture to achieve a pH of 6.4. The resulting composition is set forthbelow:

Ingredients Wt. gm Wt. % Microencapsulated composition 121.0 89.90Aluminum compound 2.8 2.08 Distilled water 10.0 7.50 Hyamine 1.7 0.5220% solution NaOH to pH 6.4 134.5 100.00

The aluminum compound used in this example as well as in examples 2-5was aluminum zirconian tetrachlorohydroxy gly having aluminum tozirconium ratio of about 3.40 to 3.80.

Following the same procedure in Example 1, four additional formulationswere prepared having the following compositions:

Example 2

Ingredients Wt. gm Wt. % Microencapsulated composition 100 82.64Aluminum compound 4.6 3.80 Distilled water 14.2 11.75 Hyamine 2.21 1.8120% solution NaOH to pH 6.4 121 100.00

Example 3

Ingredients Wt. gm Wt. % Microencapsulated composition 87.5 74.21Aluminum compound 3.5 2.96 Distilled water 10 8.49 Hyamine 0.9 .77Trehalose hydrous sigma corp 16.0 13.57 20% solution NaOH to pH 6.4117.9 100.00

Example 4

Ingredients Wt. gm Wt. % Microencapsulated composition 88 85.93 Aluminumcompound 3.5 3.41 Distilled water 10 9.76 Hyamine 0.5 .90 20% solutionNaOH to pH 6.4 102 100.00

Example 5

Ingredients Wt. gm Wt. % Microencapsulated composition 121 89.83Aluminum compound 2.8 2.08 Distilled water 10 7.42 Hyamine .9 .67 20%solution NaOH to pH 6.4 134.7 100.00

The foregoing compositions were tested clinically for theiranti-sweating efficacy and the results are discussed below.

All volunteers were instructed not to use antiperspirants, deodorants orbath salts for (48) hours prior to the test. They were also instructedto wash their body clean by shower or bath. Each was instructed to applyby hand a generous amount of the composition to the normally sweaty skinarea.

Results for example 1: Three male volunteers ages 25, 36 and 40 appliedthe compositions to each axilla of their armpit and to their foreheadbefore exercising. After jogging for three miles each reported minimalsweating.

A second test was performed on these volunteers the next day in a saunamaintained at 100° F. and 60% humidity, for 15 minutes. At the end ofthe tests their entire body was covered with sweat but their armpitswere dry.

Results of example 2: Four volunteers, three males, ages 29, 33 and 35and one female age 35 were tested. The three males jogged for threemiles and the female jogged for one mile. All had applied a generousamount of the composition to their underarms. No sweating was reportedby any of the volunteers.

Clinical tests were also conducted on other volunteers using thecompositions of the other examples with substantially the same resultsconfirming either no sweating or minimal amount of sweating whenapplying the compositions to the normally sweaty area after exercise.

In the foregoing detailed description and the illustrative examples, theingredients of the composition of this invention have been describedwith a certain degree to specificity, both as to the type of ingredientsas well as the quantity of each ingredients. It is to be understood,however that the amount of said ingredient may vary within effectiverange, and the other known equivalent ingredients may be substituted forthose specifically mentioned. Thus, when no aluminum compound is used,the amounts of the different ingredients can vary as set forth below,all percentages being on weight basis.

Trehalose about 2 to about 4% Dimethicone about 1 to about 8% Ultrex 10about 1 to about 3% Tetra sodium EDTA about 1 to about 2% Sorbitanmonolaurate about 2 to about 3% Cocoa butter about 1.2 to about 2.5%Polysorbate 20 about 0.6 to about 0.9% Germal about 0.1 to about 3%Hyamine about 1 to about 3% Bovine Collagen 2% aqueous about 1 to about3% Elastin 2% aqueous about 0.5 to about 4% Distilled water sufficientto 100%

-   -   Add 10% to NaOH solution to pH of about 6-7, preferably about        6.4

When using aluminum-zirconium compound in the composition, the amount ofthis compound may vary from about 1 to about 4 weight percent of thecomposition.

As it was previously mentioned the encapsulated trehalose is formedseparately and thereafter mixed with the remaining ingredients. Insteadof sodium alginate, other soluble salts of alginate may be used such as,e.g., potassium or amonium alginate. Also, instead of calcium chloride,other water soluble calcium salts can be used.

Other ingredients of the composition may vary. For example, instead ofsorbitan monolaurate be substituted by sorbitan monopalmitate, sorbitanmonostearate, sorbitan tristearate, sorbitan monooleate, sorbitansesquioleate, sorbitan trioleate; cocoa butter may be substituted bycocoa powder, olive oil, beeswax, having aloe; bovine collagen may besubstituted by marine collagen or ATP (adenine triphosphate, disodiumEDTA and trisodium EDTA may be used in lieu of tetra sodium EDTA; andthe following may be substituted for carbopol ultrex 10 thickener; nonbenzene carbopol polymer such as carbopol 5984 and ultrex 10 NFpolymers, carbopol 974P NF polymer, carbopol 980 NF and ultrex 10 NFpolymers, carbopol 71G NF, 971P NF and 981 NF polymers, pemulen TR-1 andTR-2 NF polymers or benzene grade carbopol polymers such as carbopol 934NF polymer, carbopol 934P NF polymer, carbopol 940 NF polymer, carbopol941 NF polymer, carbopol 1342 NF polymer.

Substitution of different ingredients for those specified in theforegoing composition are generally known to those skilled in the artfrom the detailed description.

1. A topical drying composition consisting essentially of: (a) aneffective amount of trehalose in the form of trehalose-containing gelledcalcium alginate particles dispersed within droplets of silicone oil inwhich said trehalose-containing calcium alginate particles areencapsulated and contained within said droplets of silicone oil, andwherein said droplets of silicone oil are themselves dispersed within anaqueous phase external to said droplets of silicone oil, (b) from about1 to about 5 weight percent of sorbitan monolaurate, (c) from about 0.5to about 2.5 weight percent polysorbate 20, (d) from about 1 to about 3weight percent benzethonium chloride, (e) an acceptable carrier for saidcomposition, and (f) a pH adjuster to adjust the pH of said compositionbetween about 5.5 to about 7.0.
 2. A topical drying composition as inclaim 1 wherein the pH of said composition is between about 6.0 andabout 6.6.
 3. A topical drying composition as in claim 1 wherein saidcarrier is sterilized water.
 4. A topical drying composition as in claim2 wherein said carrier is distilled water.
 5. A topical dryingcomposition as in claim 1 further including from about 0.1 to about 4.0weight percent carboxy polymethylene and from about 0.1 to about 0.6weight percent tetra sodium ethylene diamine tetra acetic acid.
 6. Atopical drying composition as in claim 2 further including from about0.1 to about 4.0 weight percent carboxy polymethylene and from about 0.1to about 0.6 weight percent tetra sodium ethylene diamine tetra aceticacid.
 7. A topical drying composition as in claim 3 further includingfrom about 0.1 to about 4.0 weight percent carboxy polymethylene andfrom about 0.1 to about 0.6 weight percent tetra sodium ethylene diaminetetra acetic acid.
 8. A topical drying composition as in claim 4 furtherincluding from about 0.1 to about 4.0 weight percent carboxypolymethylene and from about 0.1 to about 0.6 weight percent tetrasodium ethylene diamine tetra acetic acid.
 9. A topical composition asin claim 1 further including an aluminum-zirconium compound wherein theratio of aluminum to zirconium is from about 3.4 to about 3.8, and theamount of aluminum in the composition is from about 1 to about 10 weightpercent.
 10. A topical composition as in claim 2 further including analuminum-zirconium compound wherein the ratio of aluminum to zirconiumis from about 3.4 to about 3.8, and the amount of aluminum in thecomposition is from about 1 to about 10 weight percent.
 11. A topicalcomposition as in claim 3 further including an aluminum-zirconiumcompound wherein the ratio of aluminum to zirconium is from about 3.4 toabout 3.8, and the amount of aluminum in the composition is from about 1to about 10 weight percent.
 12. A topical composition as in claim 4further including an aluminum-zirconium compound wherein the ratio ofaluminum to zirconium is from about 3.4 to about 3.8, and the amount ofaluminum in the composition is from about 1 to about 10 weight percent.13. A topical composition as in claim 2 further including analuminum-zirconium compound wherein the ratio of aluminum to zirconiumis from about 3.4 to about 3.8, and the amount of aluminum in thecomposition is from about 1 to about 10 weight percent.
 14. A topicalcomposition as in claim 6 further including an aluminum-zirconiumcompound wherein the ratio of aluminum to zirconium is from about 3.4 toabout 3.8, and the amount of aluminum in the composition is from about 1to about 10 weight percent.
 15. A topical composition as in claim 7further including an aluminum-zirconium compound wherein the ratio ofaluminum to zirconium is from about 3.4 to about 3.8, and the amount ofaluminum in the composition is from about 1 to about 10 weight percent.16. A topical composition as in claim 2 further including analuminum-zirconium compound wherein the ratio of aluminum to zirconiumis from about 3.4 to about 3.8, and the amount of aluminum in thecomposition is from about 1 to about 10 weight percent.
 17. A method ofabsorbing perspiration, the method comprising applying the topicaldrying composition of claim 1 to a surface of a user's skin, whereinperspiration emitted thereafter through the surface of the user's skinis absorbed by the topical drying composition.